Assay Detail
Binding
CHEMBL954628
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flumazenil from rat GABA-A alpha-5-beta-3-gamma-2 receptor expressed in HEK293 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA A receptor alpha-5/beta-3/gamma-2 (CHEMBL2111374) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.55 | 8.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.01 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 7.46 |
| CHEMBL74302 | — | — | 1 | 7.24 |
| CHEMBL521901 | — | — | 1 | 7.02 |
| CHEMBL75306 | — | — | 1 | 6.90 |
| CHEMBL127135 | — | — | 1 | 6.79 |
| CHEMBL75456 | — | — | 1 | 6.62 |
| CHEMBL495634 | — | — | 1 | 6.60 |
| CHEMBL495616 | — | — | 1 | 6.13 |
| CHEMBL495615 | — | — | 1 | 5.85 |
| CHEMBL495592 | — | — | 1 | 5.67 |
| CHEMBL307139 | — | — | 1 | 5.65 |
| CHEMBL75406 | — | — | 1 | 5.26 |
| CHEMBL522888 | — | — | 1 | - |
| CHEMBL522059 | — | — | 1 | - |
| CHEMBL496228 | — | — | 1 | - |
| CHEMBL339918 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL74302 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL521901 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL75306 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL127135 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL75456 | — | Ki | = | 239.0 | nM | 6.62 |
| CHEMBL495634 | — | Ki | = | 252.0 | nM | 6.60 |
| CHEMBL495616 | — | Ki | = | 749.0 | nM | 6.13 |
| CHEMBL495615 | — | Ki | = | 1420.0 | nM | 5.85 |
| CHEMBL495592 | — | Ki | = | 2160.0 | nM | 5.67 |
| CHEMBL307139 | — | Ki | = | 2220.0 | nM | 5.65 |
| CHEMBL75406 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL522888 | — | Ki | - | — | - | |
| CHEMBL522059 | — | Ki | - | — | - | |
| CHEMBL496228 | — | Ki | - | — | - | |
| CHEMBL339918 | — | Ki | - | — | - |